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Nampt-IN-5 is a potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 also inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively .
Nampt degrader-2 is a fluorescent PROTAC, which efficiently degrades NAMPT with an IC50 of 41.9 nM. Nampt degrader-2 binds to NAMPT and VHL to form a ternary complex and subsequently induced NAMPT degradation via ubiquitin-proteasome system (UPS). Nampt degrader-2 leads to significant reduction of NAD + and exerts potent antitumor activities .
NAMPT activator-3, a NAT derivative, is a NAMPT activator with an EC50 of 2.6 μM and a KD of 132 nM. NAMPT activator-3 effectively protects cultured cells from FK866 (HY-50876)-mediated toxicity. NAMPT activator-3 exhibits strong neuroprotective efficacy in a chemotherapy-induced peripheral neuropathy (CIPN) mouse model without any overt toxicity .
Nampt-IN-14 (example 3) is a potent NAMPT inhibitor with an IC50 of 0.2 nM. Nampt-IN-14 can be used in the synthesis of Antibody-drug Conjugate (ADC) .
Nampt-IN-7 (compound GF8) is a potent NAMPT inhibitor, with an IC50 of 7.31 μM. Nampt-IN-7 also displays cytotoxic activity against human HepG2 hepatocellular carcinoma cell line with an IC50 of 24.28 μM .
Nampt-IN-8 (Compound 10d) is an NAMPT inhibitor with an IC50 of 0.183 μM. Nampt-IN-8 is also a relatively good NQO1 substrate. Nampt-IN-8 induces cell apoptosis and ROS .
NAMPT activator-7 (Compound 232) is an activator for nicotinamide phosphoribosyltransferase (NAMPT), with EC50 < 0.5 μM. NAMPT activator-7 activates NAMPT in cells U2OS with cellular EC50 of < 0.5 μM .
NAMPT activator-8 (Compound 278) is an activator for nicotinamide phosphoribosyltransferase (NAMPT), with EC50 < 0.5 μM. NAMPT activator-8 activates NAMPT in cells U2OS with cellular EC50 of < 0.5 μM .
NAMPT activator-6 is a NAMPT activator, a regulatory molecule for the optical control system of NAMPT and NAD+. NAMPT activator-6 can be used to design efficient photoswitchable proteolysis-targeting chimeras (PS-PROTACs) to achieve up-down reversible regulation of NAMPT and NAD+ in a light-dependent manner and reduce the toxicity associated with inhibitor-based PS-PROTACs. PS-PROTAC can be used to achieve antitumor activity, NAMPT, and NAD+ modulation in vivo via optical manipulation .
NAMPT degrader-1 (Compound A3) is an nicotinamide phosphoribosyltransferase (NAMPT) degrader with an IC50 of 0.023 μM. NAMPT degrader-1 significantly induces the degradation of NAMPT through the autophagy-lysosomal pathway and shows excellent cellular antitumor potency .
Nampt activator-5 (compound C8) is a potent nicotinamide phosphoribosyltransferase (NAMPT) activator with a KD value of 6.19 µM. Nampt activator-5 shows a cellular antisenescence effect. Nampt activator-5 promotes the production of NAD + in the brain and reduces the expression of age-related markers and secretory phenotypes. Nampt activator-5 has the potential for the research of age-related diseases .
NAMPT degrader-3 (compound C5) is a NAMPT degrader, depending on VHL- and proteasome manner. NAMPT degrader-3 displays cytotoxicity and inhibits A2780 cells proliferation .
Nampt-IN-10 trihydrochloride (compound 4) is a Nicotinamide Phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-10 trihydrochloride shows cellular potency to A2780 and CORL23 cell lines with IC50 values of 5 and 19 nM, respectively. Nampt-IN-10 trihydrochloride can be used as a novel non-antimitotic payload for antibody-drug conjugate (ADC) .
Nampt activator-4 is a positive allosteric modulator (N-PAM) of nicotinamide phosphoribosyltransferase (NAMPT) with an EC50 of 0.058 μM. Nampt activator-4 can enhance the nicotinamide adenine dinucleotide (NAD +) in cells .
Nampt-IN-3 (Compound 35) simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC with IC50s of 31 nM and 55 nM, respectively. Nampt-IN-3 effectively induces cell apoptosis and autophagy and ultimately leads to cell death .
Nampt-IN-10 TFA (compound 4) is a Nicotinamide Phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-10 TFA shows cellular potency to A2780 and CORL23 cells lines with IC50s of 5 and 19 nM, respectively. Nampt-IN-10 TFA can be used as a novel non-antimitotic payload for ADCs .
Nampt-IN-15 (Example 3) is an Nampt inhibitor. Nampt-IN-15 shows cytotoxicity against BxPC-3, HepG2, L540cy and MOLM-13, with IC50s of 38.5 nM, 8 nM, 8.5 nM, 7 nM respectively .
Nampt-IN-12 (compound 9) is a derivative of N-Pyridinylthiophene carboxamide, exhibiting activity against peripheral nerve sheath tumor cells. Nampt-IN-12 is metabolized via the enzymes NAMPT and NMNAT1, both integral to the NAD salvage pathway, into an adenosine diphosphate (AD) derivative, which is an analog of NAD and capable of inhibiting inosine monophosphate dehydrogenase (IMPDH), leading to the accumulation of inosine monophosphate (IMP) within cells. With its favorable ability to cross the blood-brain barrier, Nampt-IN-12 holds potential for research in cancers affecting both the central and peripheral nervous systems .
NAMPT/IDO1-IN-1 is an orally active dual inhibitor of NAMPT and IDO1 with IC50s of 57.7 nM and 233 nM, respectively. NAMPT/IDO1-IN-1 blocks NAD+ biosynthesis, inhibits proliferation and migration of Paclitaxel (HY-B0015)- and FK866 (HY-50876)-resistant NSCLC cell lines (A549/R cells). NAMPT/IDO1-IN-1 has shown antitumor effects in mice and enhanced A549/R cell sensitivity to paclitaxel .
NAMPT Human Pre-designed siRNA Set A contains three designed siRNAs for NAMPT gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Nampt Mouse Pre-designed siRNA Set A contains three designed siRNAs for Nampt gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Nampt Rat Pre-designed siRNA Set A contains three designed siRNAs for Nampt gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
NAMPT inhibitor-linker 2 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
NAMPT inhibitor-linker 1 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
PROTAC NAMPT Degrader-1 is a potent PROTAC targeting NAMPT with aDC50 value of 217 nM. PROTAC NAMPT Degrader-1 has anti-proliferative activity with an IC50 value of 0.12μM against A2780 cells.
(Srtucture Note: PINK, NAMPT activator (HY-163445); Blue, VHL ligand (HY-163440); Black, linker) .
BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC50=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 inhibits the growth and migration of hepatocellular carcinoma cells and promotes apoptosis. BRD4/NAMPT-IN-1 also shows potent anticancer effects in HCCLM3 xenograft mouse model, with no obvious toxic effects .
NAT is an initial hit of NAMPT activator. NAMPT is the rate-limiting enzyme in the NAD salvage pathway, which makes it an attractive target for the research of many diseases associated with NAD exhaustion such as neurodegenerative diseases .
MS7 is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT).NAMPT is the rate-limiting enzyme in the NAD + biosynthetic pathway, responsible for converting nicotinamide to nicotinamide mononucleotide, which is then converted to NAD +. NAMPT is overexpressed in many cancer cells to meet the continuous replenishment of NAD + required for rapid proliferation. PROTAC A7, a derivative of MS7, is an effective NAMPT degrader. MS7 can be used in cancer research .
(E/Z)-Daporinad hydrochloride ((E/Z)-FK866 hydrochloride) is a potent inhibitor of nicotinamide phosphoribose transferase (NAMPT). (E/Z)-Daporinad hydrochloride induces apoptosis by specifically inhibiting NAMPT to gradually deplete intracellular NAD +. (E/Z)-Daporinad hydrochloride can be used in the study of cancer biology and inflammatory diseases .
A-1293201 is a substrate-independent NAMPT inhibitor with antitumor activity. A-1293201 effectively reduces the total cellular NAD +/NADH (NADt) level, subsequently leading to ATP depletion and cancer cell death. In addition, A-1293201 can effectively overcome the acquired resistance mechanism of the NAMPT Y18 mutant to CHS-828 (HY-10079) .
CB30865 (ZM 242421) is a nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with potent cytotoxicity. CB30865 is highly potent against a variety of human tumour cell lines (IC50 values in the 1-10 nM range) .
Teglarinad chloride (GMX1777) is a proagent of GMX1778 (a nicotinamide phosphoribosyl transferase inhibitor). Teglarinad chloride exhibits antitumor activity in mice can be attributed to inhibition of NAMPT. Teglarinad chloride also enhances radiation efficacy, mediated by interference with DNA repair and antiangiogenesis .
SBI-797812 is an orally active nicotinamide phosphoribosyltransferase (NAMPT) activator. SBI-797812 shifts NAMPT to NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD +. SBI-797812 increases intracellular nicotinamide mononucleotide (NMN) and elevates liver NAD + in mice .
GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
GNE-617 hydrochloride is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
LYP-8 is a potent and effective NAMPT degrader with maximum degradation of 97% at 0.5 μM in SKOV-3 cells. LYP-8 shows anti-cancer activity in vivo and in vitro(Sturcture Note:(Blue: Cereblon ligand (HY-112078), Black: linker (HY-128801)；Pink: Nampt inhibitor Nampt-IN-11 (HY-158689)) .
LZFPN-90 (LZ90) is a dual NAMPT/PD-L1 targeting compound. LZFPN-90 inhibits PD-1/PD-L1 interaction and NAMPT activity. LZFPN-90 inhibits cell growth in a NAMPT-dependent manner and blocks the cell cycle, subsequently inducing apoptosis. LZFPN-90 exerted target-dependent antitumor activities, affecting metabolic processes and the immune system .
Antitumor Agent-136 (Compound 17) is a potent broad-spectrum antitumor agent and a NAMPT inhibitor with an IC50 of 9.5 nM. Antitumor Agent-136 can reduce the levels of intracellular and extracellular NAMPT protein through the ubiquitin proteasome pathway, thus achieving tumor inhibition .
Padnarsertib (KPT-9274) is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase(Nampt) inhibitor, with IC50s of <100 nM and 120 nM, respectively .
m-PEG6-Lys-Mal-Toxophore-quinoline is a drug-linker conjugate for ADC and can be used for ADC synthesis. The payload is a NAMPT inhibitor (HY-164760) .
LB-60-OF61 hydrochloride is a potent NAMPT (nicotinamide phosphoribosyltransferase) inhibitor. LB-60-OF61 hydrochloride is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines .
GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC50 of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity .
CHS-828 (GMX1778) is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC50 less than 25 nM. CHS-828 (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD + and exhibits a potent anticancer activity .
CHS-828 nicotinate is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC50 less than 25 nM. CHS-828 nicotinate (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD + and exhibits a potent anticancer activity .
STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1 μM. STF-31 is also a NAMPT inhibitor. STF-31 inhibits glucose uptake in renal cell carcinoma (RCC) 4 cells .
β-nicotinamide mononucleotide (β-NM) is a product of the nicotinamide phosphoribosyltransferase (NAMPT) reaction and a key NAD + intermediate. The pharmacological activities of β-nicotinamide mononucleotide include its role in cellular biochemical functions, cardioprotection, diabetes, Alzheimer's disease, and complications associated with obesity .
OT-82 is a potent, selective and orally active inhibitor of NAMPT. OT-82 is selectively toxic to cells of hematopoietic origin and induces cell death in a NAD + dependent manner. OT-82 is a promising antineoplastic agent for the study of hematological malignancies .
GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects .
β-Nicotinamide mononucleotide-d4 is the deuterium labeled β-Nicotinamide mononucleotide. β-nicotinamide mononucleotide (β-NM) is a product of the nicotinamide phosphoribosyltransferase (NAMPT) reaction and a key NAD+ intermediate. The pharmacological activities of β-nicotinamide mononucleotide include its role in cellular biochemical functions, cardioprotection, diabetes, Alzheimer's disease, and complications associated with obesity[1].
JGB-1-155 is a positive allosteric modulators (N-PAMs), which enhances the activity of nicotinamide phosphoribosyltransferase NAMPT with EC50 of 3.29 μM. JGB-1-155 counteracts the oxidative stress, through upregulating the NAD + in THP-1 human monocytes. JGB-1-155 attenuates TNFα-induced ROS in HT-22 cells .
β-nicotinamide mononucleotide (β-NM) is a product of the nicotinamide phosphoribosyltransferase (NAMPT) reaction and a key NAD + intermediate. The pharmacological activities of β-nicotinamide mononucleotide include its role in cellular biochemical functions, cardioprotection, diabetes, Alzheimer's disease, and complications associated with obesity .
NAMPT protein catalyzes the synthesis of nicotinamide mononucleotide, a key intermediate in NAD biosynthesis. NAMPT Protein, Human (His) is the recombinant human-derived NAMPT protein, expressed by E. coli , with N-6*His labeled tag. The total length of NAMPT Protein, Human (His) is 491 a.a., with molecular weight of 55-57 kDa.
NAMPT protein has dual functions of cytokine and adipokine. Due to limited ATP activation, its secreted form lacks enzymatic activity. It catalyzes the condensation of nicotinamide and 5-phosphoribosyl-1-pyrophosphate to produce nicotinamide mononucleotide, which is critical for NAD biosynthesis. NAMPT Protein, Mouse is the recombinant mouse-derived NAMPT protein, expressed by E. coli , with tag free. The total length of NAMPT Protein, Mouse is 491 a.a., with molecular weight of 56 kDa.
NAMPT protein has dual functions of cytokine and adipokine. Due to limited ATP activation, its secreted form lacks enzymatic activity. It catalyzes the condensation of nicotinamide and 5-phosphoribosyl-1-pyrophosphate to produce nicotinamide mononucleotide, which is critical for NAD biosynthesis. NAMPT Protein, Mouse (P.pastoris, His) is the recombinant mouse-derived NAMPT protein, expressed by P. pastoris , with N-10*His labeled tag. The total length of NAMPT Protein, Mouse (P.pastoris, His) is 491 a.a., with molecular weight of 57.9 kDa.
β-Nicotinamide mononucleotide-d4 is the deuterium labeled β-Nicotinamide mononucleotide. β-nicotinamide mononucleotide (β-NM) is a product of the nicotinamide phosphoribosyltransferase (NAMPT) reaction and a key NAD+ intermediate. The pharmacological activities of β-nicotinamide mononucleotide include its role in cellular biochemical functions, cardioprotection, diabetes, Alzheimer's disease, and complications associated with obesity[1].
Nampt Antibody (YA1183) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1183), targeting Nampt. Nampt Antibody (YA1183) can be used for IHC-P experiment in human background.
NAMPT Human Pre-designed siRNA Set A contains three designed siRNAs for NAMPT gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Nampt Mouse Pre-designed siRNA Set A contains three designed siRNAs for Nampt gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Nampt Rat Pre-designed siRNA Set A contains three designed siRNAs for Nampt gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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